Diastereoselective synthesis of hydroxyethylene dipeptide isoste

Details Diastereoselective synthesis of hydroxyethylene dipeptide isoste Diastereoselective synthesis of hydroxyethylene dipeptide isoste

1993-11-08

1996-12-24

O'Sullivan, Peter

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

2609982, 530331, 549321, 560 29, 560 39, 560 40, 560125, 560170, 562444, 562445, 562507, 562567, 564165, 564191, 564197, 564198, C07C23118

Patent

active

055875149

ABSTRACT:
A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)-amino(alkyl or substituted alkyl)methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.

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